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Drug Delivery

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https://www.readbyqxmd.com/read/28532223/preliminary-study-on-fabrication-characterization-and-synergistic-anti-lung-cancer-effects-of-self-assembled-micelles-of-covalently-conjugated-celastrol-polyethylene-glycol-ginsenoside-rh2
#1
Peng Li, XiaoYue Zhou, Ding Qu, Mengfei Guo, Chenyi Fan, Tong Zhou, Yang Ling
The aim of this study was to develop an amphipathic polyethylene glycol (PEG) derivative that was bi-terminally modified with celastrol and ginsenoside Rh2 (Celastrol-PEG-G Rh2). Such derivative was capable of forming novel, celastrol-loaded polymeric micelles (CG-M) for endo/lysosomal delivery and thereby synergistic treatment of lung cancer. Celastrol-PEG-G Rh2 with a yield of 55.6% was first synthesized and characterized. Its critical micellar concentration was 1 × 10(-5 )M, determined by pyrene entrapment method...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28509629/nanoparticle-based-delivery-enhances-anti-inflammatory-effect-of-low-molecular-weight-heparin-in-experimental-ulcerative-colitis
#2
Tawfek Yazeji, Brice Moulari, Arnaud Beduneau, Valentin Stein, Dirk Dietrich, Yann Pellequer, Alf Lamprecht
Epithelial administration of low molecular weight heparin (LMWH) has proven its therapeutic efficiency in ulcerative colitis (UC) but still lacks of a sufficiently selective drug delivery system. Polymeric nanoparticles were used here not only to protect LMWH from intestinal degradation but also to provide targeted delivery to inflamed tissue in experimental colitis mice. LMWH was associated with polymethacrylate nanoparticles (NP) type A (PEMT-A) or type B (PEMT-B) of a size: 150 nm resulting in a maximum drug loading: 0...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28509588/peg-lipid-plga-hybrid-nanoparticles-loaded-with-berberine-phospholipid-complex-to-facilitate-the-oral-delivery-efficiency
#3
Fei Yu, Mingtao Ao, Xiao Zheng, Nini Li, Junjie Xia, Yang Li, Donghui Li, Zhenqing Hou, Zhongquan Qi, Xiao Dong Chen
The natural product berberine (BBR), present in various plants, arouses great interests because of its numerous pharmacological effects. However, the further development and application of BBR had been hampered by its poor oral bioavailability. In this work, we report on polymer-lipid hybrid nanoparticles (PEG-lipid-PLGA NPs) loaded with BBR phospholipid complex using a solvent evaporation method for enhancing the oral BBR efficiency. The advantage of this new drug delivery system is that the BBR-soybean phosphatidylcholine complex (BBR-SPC) could be used to enhance the liposolubility of BBR and improve the affinity with the biodegradable polymer to increase the drug-loading capacity and controlled/sustained release...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28509581/dexamethasone-distribution-characteristic-following-controllable-continuous-sub-tenon-drug-delivery-in-rabbit
#4
Xuetao Huang, Manqiang Peng, Yezhen Yang, Yiqin Duan, Kuanshu Li, Shaogang Liu, Changhua Ye, Ding Lin
Drug delivery systems are required to be safe, minimally invasive and effectively delivery drug to the target tissues. But delivery drugs to the eye has not yet satisfied this need. Here, we focused on examining the distribution of dexamethasone (DEX) in ocular and plasmic samples following controllable continuous sub-Tenon drug delivery (CCSDD) of dexamethasone disodium phosphate (DEXP) in rabbit, and to compare that with two traditional routes: subconjunctival injection and intravenous injection. The DEX concentration was analyzed by Shimadzu LC-MS 2010 system...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28502199/ceramide-lipid-based-nanosuspension-for-enhanced-delivery-of-docetaxel-with-synergistic-antitumor-efficiency
#5
Tianqi Wang, Lixia Feng, Shaomei Yang, Yongjun Liu, Na Zhang
Ceramide (CE), a bioactive lipid with tumor suppression, has been widely used as a drug carrier and enhancer for cancer therapy. CE-based combination therapy was prone to be attractive in cancer therapy. In our previous study, the combination of CE and docetaxel (DTX) was proved to be an effective strategy for cancer therapy. To further improve the antitumor efficiency of DTX, the CE lipid-based nanosuspensions (LNS) was prepared for the delivery of DTX to exhibit synergistic therapeutic effect. The enhanced delivery and synergistic therapeutic effect of DTX-loaded CE-LNS (CE + DTX-LNS) were evaluated...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28480758/loratadine-bioavailability-via-buccal-transferosomal-gel-formulation-statistical-optimization-in-vitro-in-vivo-characterization-and-pharmacokinetics-in-human-volunteers
#6
Mohammed H Elkomy, Shahira F El Menshawe, Heba A Abou-Taleb, Marwa H Elkarmalawy
Loratadine (LTD) is an antihistaminic drug that suffers limited solubility, poor oral bioavailability (owing to extensive first-pass metabolism), and highly variable oral absorption. This study was undertaken to develop and statistically optimize transfersomal gel for transbuccal delivery of LTD. Transfersomes bearing LTD were prepared by conventional thin film hydration method and optimized using sequential Quality-by-Design approach that involved Placket-Burman design for screening followed by constrained simplex-centroid design for optimization of a Tween-80/Span-60/Span-80 mixture...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28475414/characterization-and-antitumor-efficacy-of-poly-l-lactid-acid-based-etoposide-loaded-implants
#7
Li Gao, Chuanqi Xie, Yuzhi Du, Xiaodong Wang, Erkang Xuan, Xiuxiu Liu, Yang Zhao, Jianjian Xu, Lan Luo
Etoposide is widely used in the chemotherapy of a variety of malignancies. But the strong lipophilicity, poor bioavailability, and severe side effects of etoposide limit its clinical application. The aim of this study was to develop sustained-release etoposide-loaded implants and evaluate antitumor activity of the implants after intratumoral implantation. We prepared the implants containing etoposide, poly(L-lactid acid) and polyethylene glycol 4000 by the direct compression method. The implants were characterized regarding drug-excipient compatibility, content uniformity, morphology, sterility, in vitro, and in vivo release profiles...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28475387/photonic-crystal-materials-and-their-application-in-biomedicine
#8
Huadong Chen, Rong Lou, Yanxiao Chen, Lili Chen, Jingya Lu, Qianqian Dong
Photonic crystal (PC) materials exhibit unique structural colors that originate from their intrinsic photonic band gap. Because of their highly ordered structure and distinct optical characteristics, PC-based biomaterials have advantages in the multiplex detection, biomolecular screening and real-time monitoring of biomolecules. In addition, PCs provide good platforms for drug loading and biomolecule modification, which could be applied to biosensors and biological carriers. A number of methods are now available to fabricate PC materials with variable structure colors, which could be applied in biomedicine...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28468542/cell-penetrating-peptide-conjugates-to-enhance-the-antitumor-effect-of-paclitaxel-on-drug-resistant-lung-cancer
#9
Ziqing Duan, Cuitian Chen, Jing Qin, Qi Liu, Qi Wang, Xinchun Xu, Jianxin Wang
To conquer the drug resistance of tumors and the poor solubility of paclitaxel (PTX), two PTX-cell-penetrating peptide conjugates (PTX-CPPs), PTX-TAT and PTX-LMWP, were synthesized and evaluated for the first time. Compared with free PTX, PTX-CPPs displayed significantly enhanced cellular uptake, elevated cell toxicity, increased cell apoptosis, and decreased mitochondrial membrane potential (Δψm) in both A549 and A549T cells. PTX-LMWP exhibited a stronger inhibitory effect than PTX-TAT in A549T cells. Analysis of cell-cycle distribution showed that PTX-LMWP influenced mitosis in drug-resistant A549T tumor cells via a different mechanism than PTX...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28454494/preparation-and-testing-of-cefquinome-loaded-poly-lactic-co-glycolic-acid-microspheres-for-lung-targeting
#10
Shaoqi Qu, Li Zhao, Jiajia Zhu, Chunmei Wang, Cunchun Dai, Hui Guo, Zhihui Hao
The aim of this study was to prepare cefquinome-loaded poly lactic-co-glycolic acid (PLGA) microspheres and to evaluate their in vitro and in vivo characteristics. Microspheres were prepared using a spry drier and were characterized in terms of morphology, size, drug-loading coefficient, encapsulation ratio and in vitro release. The prepared microspheres were spherical with smooth surfaces and uniform size (12.4 ± 1.2 μm). The encapsulation efficiency and drug loading of cefquinome was 91.6 ± 2...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28446052/effective-intraperitoneal-gene-transfection-system-using-nanobubbles-and-ultrasound-irradiation
#11
Koyo Nishimura, Shintaro Fumoto, Yuki Fuchigami, Masayori Hagimori, Kazuo Maruyama, Shigeru Kawakami
In this study, we demonstrate the low toxicity and highly efficient and spatially improved transfection of plasmid DNA (pDNA) with liposomal nanobubbles (bubble liposomes [BLs]) using ultrasound (US) irradiation in mice. Naked pDNA with BLs was intraperitoneally injected, followed by US irradiation. The injection volume, the duration of US irradiation, and the dose of BLs were optimized. Both BLs and US irradiation were essential to achieve high transgene expression from naked pDNA. We observed transgene expression in the entire peritoneal tissues, including the peritoneal wall, liver, spleen, stomach and small and large intestines...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28440691/n-butyl-2-cyanoacrylate-based-injectable-and-in-situ-forming-implants-for-efficient-intratumoral-chemotherapy
#12
Yanpu Wu, Luming Wang, Kaili Zhang, Lixiao Zhou, Xiaobing Zhang, Xuecheng Jiang, Chenggang Zhu
The local delivery of chemotherapeutic drugs to tumor sites is an effective approach for achieving therapeutic drug concentrations in solid tumors. Injectable implants with the ability to form in situ represent one of the most promising technologies for intratumoral chemotherapy. However, many issues must be resolved before these implants can be applied in clinical practice. Herein, we report a novel injectable in situ-forming implant system composed of n-butyl-2-cyanoacrylate (NBCA) and ethyl oleate, and the sol-gel phase transition is activated by anions in body fluids or blood...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28436718/design-of-a-novel-curcumin-soybean-phosphatidylcholine-complex-based-targeted-drug-delivery-systems
#13
Jiajiang Xie, Yanxiu Li, Liang Song, Zhou Pan, Shefang Ye, Zhenqing Hou
Recently, the global trend in the field of nanomedicine has been toward the design of combination of nature active constituents and phospholipid (PC) to form a therapeutic drug-phospholipid complex. As a particular amphiphilic molecular complex, it can be a unique bridge of traditional dosage-form and novel drug delivery system. In thisarticle, on the basis of drug-phospholipid complex technique and self-assembly technique, we chose a pharmacologically safe and low toxic drug curcumin (CUR) to increase drug-loading ability, achieve controlled/sustained drug release and improve anticancer activity...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28436702/a-novel-matrix-dispersion-based-on-phospholipid-complex-for-improving-oral-bioavailability-of-baicalein-preparation-in-vitro-and-in-vivo-evaluations
#14
Yang Zhou, Wujun Dong, Jun Ye, Huazhen Hao, Junzhuo Zhou, Renyun Wang, Yuling Liu
Phospholipid complex is one of the most successful approaches for enhancing oral bioavailability of poorly absorbed plant constituents. But the sticky property of phospholipids results in an unsatisfactory dissolution of drugs. In this study, a matrix dispersion of baicalein based on phospholipid complex (BaPC-MD) was first prepared by a discontinuous solvent evaporation method, in which polyvinylpyrrolidone-K30 (PVP-K30) was employed for improving the dispersibility of baicalein phospholipid complex (BaPC) and increasing dissolution of baicalein...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28426265/transdermal-iontophoresis-patch-with-reverse-electrodialysis
#15
Joon Lee, Kilsung Kwon, Minyoung Kim, Joonhong Min, Nathaniel S Hwang, Won-Serk Kim
Reverse electrodialysis (RED) technology generates energy from the salinity gradient by contacting waters with different salinity. Herein, we develop the disposable skin patch using this eco-friendly energy. The current density, which can be controlled easily without special circuit, is enough to iontophoretic drug delivery. In vitro study, this iontophoretic system enhanced the transdermal delivery of peptide, which is difficult to penetrate the skin barrier by simple diffusion. We design the disposable iontophoretic skin patch using RED system and suggest this patch can be apply on new cosmetic patch or disposable drug patch...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28415883/electrosteric-stealth-rivastigmine-loaded-liposomes-for-brain-targeting-preparation-characterization-ex-vivo-bio-distribution-and-in-vivo-pharmacokinetic-studies
#16
Sara Nageeb El-Helaly, Ahmed Abd Elbary, Mohamed A Kassem, Mohamed A El-Nabarawi
Being one of the highly effective drugs in treatment of Alzheimer's disease, Rivastigmine brain targeting is highly demandable, therefore liposomal dispersion of Rivastigmine was prepared containing 2 mol% PEG-DSPE added to Lecithin, Didecyldimethyl ammonium bromide (DDAB), Tween 80 in 1:0.02:0.25 molar ratio. A major challenge during the preparation of liposomes is maintaining a stable formulation, therefore the aim of our study was to increase liposomal stability by addition of DDAB to give an electrostatic stability and PEG-DSPE to increase stability by steric hindrance, yielding what we called an electrosteric stealth (ESS) liposomes...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28414557/polydopamine-and-peptide-decorated-doxorubicin-loaded-mesoporous-silica-nanoparticles-as-a-targeted-drug-delivery-system-for-bladder-cancer-therapy
#17
Yi Wei, Li Gao, Lu Wang, Lin Shi, Erdong Wei, Baotong Zhou, Li Zhou, Bo Ge
We reported a simple polydopamine (PDA)-based surface modification method to prepare novel targeted doxorubicin-loaded mesoporous silica nanoparticles and peptide CSNRDARRC conjugation (DOX-loaded MSNs@PDA-PEP) for enhancing the therapeutic effects on bladder cancer. Drug-loaded NPs were characterized in terms of size, size distribution, zeta potential, transmission electron microscopy (TEM), Brunauer-Emmett-Teller (BET) surface area and drug loading content. In vitro drug release indicated that DOX-loaded MSNs@PDA and MSNs@PDA-PEP had similar release kinetic profiles of DOX...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28368209/enhanced-cytotoxic-effect-of-camptothecin-nanosponges-in-anaplastic-thyroid-cancer-cells-in-vitro-and-in-vivo-on-orthotopic-xenograft-tumors
#18
Casimiro Luca Gigliotti, Benedetta Ferrara, Sergio Occhipinti, Elena Boggio, Giuseppina Barrera, Stefania Pizzimenti, Mirella Giovarelli, Roberto Fantozzi, Annalisa Chiocchetti, Monica Argenziano, Nausicaa Clemente, Francesco Trotta, Caterina Marchiò, Laura Annaratone, Renzo Boldorini, Umberto Dianzani, Roberta Cavalli, Chiara Dianzani
Anaplastic carcinoma of the thyroid (ATC) is a lethal human malignant cancer with median survival of 6 months. To date, no treatment has substantially changed its course, which makes urgent need for the development of novel drugs or novel formulations for drug delivery. Nanomedicine has enormous potential to improve the accuracy of cancer therapy by enhancing availability and stability, decreasing effective doses and reducing side effects of drugs. Camptothecin (CPT) is an inhibitor of DNA topoisomerase-I with several anticancer properties but has poor solubility and a high degradation rate...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28368206/honokiol-loaded-polymeric-nanoparticles-an-active-targeting-drug-delivery-system-for-the-treatment-of-nasopharyngeal-carcinoma
#19
Bo Yang, XiaoLing Ni, LongXia Chen, Heng Zhang, PeiRong Ren, Yue Feng, Yue Chen, ShaoZhi Fu, JingBo Wu
The purpose of this study was to develop a novel drug delivery system for a sustained and targeted delivery of honokiol (HK) to the nasopharyngeal carcinoma (NPC) HNE-1 cell lines, since the folate receptor (FR) is over-expressed on their surface. Emulsion solvent evaporation was used to develop the active targeting nanoparticles-loaded HK (ATNH) using copolymerpoly (ɛ-caprolactone)-poly (ethyleneglycol)-poly (ɛ-caprolactone) (PCEC), which was modified with folate (FA) by introducing Polythylenimine (PEI)...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28283003/bacterial-magnetic-particles-improve-testes-mediated-transgene-efficiency-in-mice
#20
COMPARATIVE STUDY
Chao Wang, Guanghong Sun, Ye Wang, Nana Kong, Yafei Chi, Leilei Yang, Qiliang Xin, Zhen Teng, Xu Wang, Yujun Wen, Ying Li, Guoliang Xia
Nano-scaled materials have been proved to be ideal DNA carriers for transgene. Bacterial magnetic particles (BMPs) help to reduce the toxicity of polyethylenimine (PEI), an efficient gene-transferring agent, and assist tissue transgene ex vivo. Here, the effectiveness of the BMP-PEI complex-conjugated foreign DNAs (BPDs) in promoting testes-mediated gene transfer (TMGT) in mouse was compared with that of liposome-conjugated foreign DNAs. The results proved that through testes injection, the clusters of BPDs successfully reached the cytoplasm and the nuclear of spermatogenesis cell, and expressed in testes of transgene founder mice...
November 2017: Drug Delivery
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